Kev piav qhia

Lenalidomide (CC-5013) yog ib qho derivative ntawm Thalidomide thiab ib qho tshuaj tiv thaiv kab mob hauv qhov ncauj.Lenalidomide (CC-5013) yog ligand ntawm ubiquitin E3 ligase cereblon (CRBN), thiab nws ua rau xaiv ubiquitination thiab degradation ntawm ob lymphoid transcription yam, IKZF1 thiab IKZF3, los ntawm CRBN-CRL4 ubiquitin ligase.Lenalidomide (CC-5013) tshwj xeeb inhibits kev loj hlob ntawm cov laus B-cell lymphomas, nrog rau ntau yam myeloma, thiab induces IL-2 tso tawm ntawm T hlwb.

Keeb kwm

Lenalidomide (tseem hu ua CC-5013), lub qhov ncauj derivative ntawm thalidomide, yog ib tug antineoplastic tus neeg sawv cev nthuav tawm antitumor kev ua los ntawm ntau yam txheej txheem, nrog rau kev ua kom lub cev tsis muaj zog, angiogenesis inhibition, thiab ncaj qha antineoplastic cuam tshuam.Nws tau raug tshawb fawb ntau rau kev kho mob ntawm ntau yam myeloma thiab myelodysplastic syndrome nrog rau cov kab mob lymphoproliferative nrog rau cov kab mob lymphocytic leukemia (CLL) thiab non-Hodgkin lymphoma.Raws li kev tshawb fawb tsis ntev los no, Lnalidomide txhawb nqa thiab kho lub cev tiv thaiv kab mob hauv cov neeg mob CLL los ntawm kev ua rau muaj kev cuam tshuam ntau dhau ntawm costimulatory molecules hauv leukemic lymphocytes los kho cov kev tiv thaiv kab mob humoral thiab immunoglobulins ntau lawm nrog rau kev txhim kho lub peev xwm ntawm T cell thiab leukemic hlwb los tsim synapses nrog T. lymphocytes.

Kev siv

Ana Pilar Gonzalez-Rodriguez, Angel R. Payer, Andrea Acebes-Huerta, Leticia Hergo-Zapico, Monica Villa-Alvarez, Esther Gonzalez-Garcia, thiab Segundo Gonzalez.Lenalidomide thiab mob lymphocytic leukemia.BioMed Research International 2013.

Hauv Vitro

Lenalidomide muaj zog hauv stimulating T cell proliferation thiab IFN-γ thiab IL-2 ntau lawm.Lenalidomide tau pom tias inhibit zus tau tej cov pro-inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 thiab txhawb kev tsim cov tshuaj tiv thaiv cytokine IL-10 los ntawm tib neeg PBMCs.Lenalidomide downregulates zus tau tej cov IL-6 ncaj qha thiab kuj los ntawm inhibiting ntau myeloma (MM) hlwb thiab cov pob txha pob txha stromal hlwb (BMSC), uas augments lub apoptosis ntawm myeloma hlwb [2].Kev sib cuam tshuam ntawm koob tshuaj nrog CRBN-DDB1 complex yog pom nrog Thalidomide, Lenalidomide thiab Pomalidomide, nrog IC50 qhov tseem ceeb ntawm ~ 30μM, ~ 3μM thiab ~ 3μM, raws li, Cov kev txo qis CRBN nthuav qhia hlwb (U266-CRBN60 thiab U266-CRBN75) tsis tshua teb dua li cov niam txiv cov hlwb rau cov tshuaj tiv thaiv kab mob Lenalidomide thoob plaws cov tshuaj teb ntau ntawm 0.01 txog 10.μM[3].Lenalidomide, thalidomide analog, ua haujlwm raws li cov kua nplaum molecular ntawm tib neeg E3 ubiquitin ligase cereblon thiab CKIα tau pom tias ua rau muaj kev cuam tshuam rau ubiquitination thiab degradation ntawm no kinase, yog li xav tias tua cov leukemic hlwb los ntawm kev ua kom p53.

Cov tshuaj toxicity ntawm Lenalidomide koob tshuaj txog li 15, 22.5, thiab 45 mg / kg ntawm IV, IP, thiab PO txoj kev tswj hwm.Txwv tsis pub los ntawm kev solubility hauv peb lub tsheb txhaj tshuaj PBS, cov koob tshuaj Lenalidomide qhov siab tshaj plaws no tau txais txiaj ntsig zoo nrog kev zam ntawm ib tus nas tuag (ntawm plaub qhov koob tshuaj tag nrho) ntawm 15 mg / kg IV koob.Qhov tseem ceeb, tsis muaj lwm yam tshuaj toxicity tau pom nyob rau hauv txoj kev tshawb fawb ntawm IV koob tshuaj 15 mg / kg (n = 3) los yog 10 mg / kg (n = 45) los yog lwm yam koob tshuaj los ntawm IV, IP, thiab PO txoj kev.

Cia

Cov qauv tshuaj

Cov ntaub ntawv ntsig txog Biological

Cov ntaub ntawv ntsig txog Biological